Method for the immobilization of bioactive molecules within a polymeric substrate resistant to the stomach acids as oral drug delivery system

Abstract

It is described a technology which allows to surpass the gastric barrier for proteic compounds administrating bioactive molecules, particularly insulin. It is proposed a method to replace the daily repetitive injectable doses of insulin by a product oralyy administered. It is characterized by the following steps: a) mix at least a monomer suitable for polymerization by means of a ionizing radiation, with at least an aqueous solution of bioactive molecules; place the thus obtained mixture in step (a) into a resistant container permeable to said ionizing radiations; submit said container to a flow of ionizing radiation at a dose capable to polymerize all the monomer, in a dose range from 0.1 kGy up to 50 kGy, particularly in a 5 to 30 kGy in range, obtaining within the container a polymer resistant to the stomach acids. And the polymer containing in its nanotubules bioactive molecules; withdraw the thus polymer obtained in step (c), and dividing it in batches with a size range of 1 mm x 1 mm x 1 mm up to 8 mm x 8 mm x 8 mm, It is an objective of this invention. A method for the introduction of bioactive molecules in a polymeric substrate resistent to the stomach acids, to be employed as a retarding orally administered medicine, being these molecules insulin which is releaase directly to the liver being the liver its first action site, through the portal circulation; an orally relased insulin of delayed action by means of which, when the insulin is released into the liver, controls the porduction of hepatic glucose; an orally relased insulin of delayed action by means of which eht einsulin does not produce peaks in the systemic circulation, as it does with the injectable insulin, reducing the risks of the sudden descrese in the glucemia levels, an orally adminstered mediciene with a prolongued retared effect, by means of wish it is neccesary a lesser insulin dose.